MED. CHEM. I STUDY GUIDE
Quiz Two
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ANALGESICS |
- A. NARCOTIC ANALGESICS
- A. NARCOTIC ANALGESICS
- 1. Life Cycle of Enkephalinergic Neurotransmission (Diagram p. 18, Lecture Guide)
- a. Biosynthesis of the pentapeptide enkephalin from pro-opioid precursors
- b. Storage of enkephalin in presynaptic vesicles
- c. Release of enkephalin into synaptic cleft
- d. Interaction of enkephalin with postsynaptic receptors (mu, kappa and delta)
- e. Termination of enkephalinergic neurotransmission by a membrane-bound protease:
L-Tyr-Gly-Gly-L-Phe-L-Met -----------------> L-Tyr-OH + H2N-Gly-Gly-L-Phe-L-Met
- 2. General Structural Features
- a. Morphine - structural features and functions
- b. Analgesiophore structure
- c. Structural derivation of narcotic analgesics from morphine(click here for diagram)
- 1) Peripherally-modified morphine derivatives
- a) Agonists - Codeine, heroin, etc.
- b) Agonists-Antagonists - N17-substituted morphine derivatives
- 2) Ring-modified morphine derivatives
- a) Morphinans
- b) Benzomorphans
- c) Piperidines
- d) Diphenylpropylamines
d. Physicochemical Properties
- 1) Lipid solubility
- a) Access to CNS
- b) Duration of action
- 2) Basicity
- a) Ionization in vivo
- b) Reaction with acids - salt formation (dose formulation)
- 3) Structure vs. potency, onset, and duration. Click here.
L-Tyr-Gly-Gly-L-Phe-L-Met -----------------> L-Tyr-OH + H2N-Gly-Gly-L-Phe-L-Met
- 1) Peripherally-modified morphine derivatives
- a) Agonists - Codeine, heroin, etc.
- b) Agonists-Antagonists - N17-substituted morphine derivatives
- 2) Ring-modified morphine derivatives
- a) Morphinans
- b) Benzomorphans
- c) Piperidines
- d) Diphenylpropylamines
- b) Benzomorphans
- a) Agonists - Codeine, heroin, etc.
- 1) Lipid solubility
- a) Access to CNS
- b) Duration of action
- 2) Basicity
- a) Ionization in vivo
- b) Reaction with acids - salt formation (dose formulation)
- 3) Structure vs. potency, onset, and duration. Click here.
- a) Access to CNS
- a. Structural features favoring peripheral actions
- B. MILD ANALGESICS (NSAIDS)
- 1. Mechanism of action of NSAIDS
- a. Biosynthesis of chemical mediators of inflammation
- b. Inhibition of cyclooxygenase
- c. Therapeutic uses
- b. Inhibition of cyclooxygenase
- 2. Structural and chemical properties of NSAIDs
- a. Pharmacophore
- b. Acidic character of NSAIDs
- 1) Ionization at physiologic pH
- 2) Salt formation for dosage formulation
- b. Acidic character of NSAIDs
- 3. NSAID Structural classes
- a. Salicylates (reversible vs. irreversible inhibition of cyclooxygenase, biotransformation)
- b. Profens (general structural appearance, role of stereochemistry in pharmacological activity and biodisposition)
- c. Heteroarylacetic acids (general structural appearance, geometric isomerism, design of prodrugs and potential therapeutic benefits, structure vs. metabolic lability)
- d. Fenamates (structural derivation from salicylates)
- e. Oxicams (structural appearance, nature of acidic character)
- f. Pyrazolones (structural appearance, nature of acidic character)
- g. Anilides (structural appearance, metabolism and detoxification, treatment of overdosage)
- b. Profens (general structural appearance, role of stereochemistry in pharmacological activity and biodisposition)
- C. DRUGS AFFECTING AMINO ACID NEUROTRANSMISSION
- 1. Amino Acid Neurotransmitters
- a. Excitatory (L-Glu, L-Asp)
- b. Inhibitory (GABA, Gly)
- c. Structural characteristics
- b. Inhibitory (GABA, Gly)
- 2. GABA Neurotransmission
- a. Biosynthesis
- b. Storage
- c. Release
- d. Receptors (types, signal transduction)
- e. Termination, metabolism
- b. Storage
- a. Biosynthesis of chemical mediators of inflammation
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